Literature summary for 1.3.1.22 extracted from

Aggarwal, S.; Thareja, S.; Bhardwaj, T.R.; Haupenthal, J.; Hartmann, R.W.; Kumar, M.
Synthesis and biological evaluation of novel unsaturated carboxysteroids as human 5alpha-reductase inhibitors: a legitimate approach (2012), Eur. J. Med. Chem., 54, 728-739.

Search for more literature for 1.3.1.22

Cloned(Commentary)

Cloned (Comment)	Organism
transfection of HEK-293 cell	Homo sapiens

Inhibitors

Inhibitors	Comment	Organism	Structure
17a-(2-propionoxyethyl)-17-oxo-17a-aza-D-homo-3,5-androstadien-3-oic acid	0.01 mM, 100% inhibition; 0.01 mM, 8.5% inhibition	Homo sapiens
17a-allyl-17-oxo-17a-aza-D-homo-3,5-androstadien-3-oic acid	0.01 mM, 0.4% inhibition; 0.01 mM, 99% inhibition	Homo sapiens
17a-ethyl-17-oxo-17a-aza-D-homo-3,5-androstadien-3-oic acid	0.01 mM, 100% inhibition; 0.01 mM, 32.3% inhibition	Homo sapiens
17a-methyl-17-oxo-17a-aza-D-homo-3,5-androstadien-3-oic acid	0.01 mM, 18.9% inhibition; 0.01 mM, 99% inhibition	Homo sapiens

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	P18405	isoform steroid 5-alpha-reductase 1	-
Homo sapiens	P31213	isoform steroid 5-alpha-reductase 2	-

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
0.000022	-	pH not specified in the publication, 37°C	Homo sapiens	17a-ethyl-17-oxo-17a-aza-D-homo-3,5-androstadien-3-oic acid
0.000026	-	pH not specified in the publication, 37°C	Homo sapiens	17a-(2-propionoxyethyl)-17-oxo-17a-aza-D-homo-3,5-androstadien-3-oic acid
0.000054	-	pH not specified in the publication, 37°C	Homo sapiens	17a-methyl-17-oxo-17a-aza-D-homo-3,5-androstadien-3-oic acid
0.000073	-	pH not specified in the publication, 37°C	Homo sapiens	17a-allyl-17-oxo-17a-aza-D-homo-3,5-androstadien-3-oic acid

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Release 2023.1 (January 2023)